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Updated: Dec 24 2017

Elimination of Drugs

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  • Overview
    • Elimination of drugs
      • rate of elimination is rate of disappearance of active molecules from bloodstream or body
      • rate of elimination and dosage determine duration of action of a drug
      • drug elimination ≠ drug excretion
        • e.g., a drug may be eliminated by metabolism before excretion from body
  • Zero-order elimination
    • Zero-order elimination
      • implies rate of elimination is constant, regardless of drug concentration
        • constant amount of drug is eliminated per unit time
      • drug concentration in plasma (Cp) decreases linearly with time
      • e.g., phenytoin, ethanol, aspirin
        • aspirin is zero-order drug at high therapeutic or toxic concentrations
  • First-order elimination
    • First-order elimination
      • implies rate of elimination is proportional to drug concentration
        • constant fraction of drug is eliminated per unit time
      • drug concentration in plasma (Cp) decreases exponentially with time
      • first-order drugs have a characteristic, constant half-life of elimination
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